This document provides an overview of the global cancer tyrosine kinase inhibitors market and clinical pipeline outlook for 2020. It discusses tyrosine kinases' role in cancer signaling pathways and the development of tyrosine kinase inhibitors as targeted cancer therapies. The market for tyrosine kinase inhibitors is growing due to rising cancer incidence and a strong clinical pipeline. Over 400 tyrosine kinase inhibitors are in clinical development globally across various phases of trials. The future outlook for tyrosine kinase inhibitors is optimistic due to ongoing research and advancement in development approaches.

1. Global Cancer Tyrosine Kinase Inhibitors Market & Clinical Pipeline Outlook 2020
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The global increase in the prevalence of cancer and the increasing recognition of the
therapeutic and commercial opportunities offered by new oncology treatments has provided a
major incentive for the pharmaceutical industry to pursue the development of new agents for
the treatment of cancer. To tackle the ever rising global cancer burden, the cancer
treatment is inclining towards the targeted drug therapy due to the numerous drawbacks
associated with conventional chemotherapy. Targeted drug therapy includes targeting various
signaling pathways associated to the tyrosine kinase receptors. Ample of studies have been
performed which confirm their intrinsic involvement of tyrosine related pathways in
development of the tumors.
Until the late 1980s, it was thought of as impossible to target protein kinases by the tractable
drugs, the reason lied in the presumed need to compete with adenosine triphosphate (ATP) as
well as concerns regarding selectivity of the potential drugs. Since then, considerable
progress has been made, and the past few years have seen a number of kinase inhibitors
which have entered the market.
Till now, 518 protein kinases have been encoded from the human genome; we call it as
Human Kinome. From the encoded human genome, 90 kinases belong to the group of tyrosine
kinases. The tyrosine kinase group consists of approximately 30 families, for example the
VEGFR family and the fibroblast growth factor receptor (FGFR) family. Six other groups have
been identified whose kinases primarily phosphorylate serine and threonine residues.
Tyrosine kinases play the most critical part in the modulation of growth factor signaling.
Activated forms of these enzymes can cause increases in tumor cell proliferation and growth,
induce antiapoptotic effects, and promote angiogenesis and metastasis. In addition to
activation by growth factors, protein kinase activation by somatic mutation is a common
mechanism of tumor genesis. Because all of these effects are initiated by receptor tyrosine
kinase activation, they are key targets for inhibitors.
The TKI drug discovery has evolved dramatically in recent years. Along with the launch of new
drugs, efficient approaches for the development of potent and selective inhibitors with
desirable properties have become established. At present kinase inhibitors are being designed
from crystallography to deal with different binding modes and unexpected inhibitor induced
conformational rearrangements. Much of kinase inhibitors which are supposed to enter in

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market in near future are rationally designed through high throughput screening and empirical
optimization on the basis of structure–activity relationships. Sophisticated proteomic
approaches have been developed in conjunction with panels of enzyme assays to allow for a
more thorough annotation of kinase inhibitor selectivity.
Now with the considerable amount of research and advancement in technology, kinase
signaling pathway is seen as the largest class of potential drug targets by the pharmaceutical
industry. Over the last decades, billions have been spent and huge efforts have been taken in
basic and clinical cancer research. About a decade ago, the race between drugs and cancer
cells reached a new level by introduction of tyrosine kinase inhibitors into pharmacological
anti-cancer therapy.
Clinical pipeline of cancer tyrosine kinase inhibitor therapeutics is quite strong due to which
competitive product is expected to enter continuously in global market. Owing to increasing
cancer incidences, it has become imperative to take necessary steps to introduce innovative
tyrosine kinase inhibitor therapeutics in global market. Technological advancements may
allow the investigators to develop products having high safety and efficacy levels along with
minimized side effects but it will take some time. Various products are at different stages of
clinical trials which will be introduced in global market in coming years. Higher cost
effectiveness is expected due to which sales is expected to increase and profit margins will
increase. With all these development, the future of tyrosine kinase therapeutics looks
optimistic.
“Global Cancer Tyrosine Kinase Inhibitors Market & Clinical Pipeline Outlook
2020” Report Highlights:
• Introduction to Cancer Tyrosine Kinase Inhibitors
• Signaling Pathway of Receptor Tyrosine Kinase
• Advantage of Tyrosine Kinase Inhibitors for Treatment of Cancer
• Applications of Tyrosine Kinase Inhibitor in Cancer Therapy
• Global Tyrosine Kinase Inhibitors Market Overview
• Global Cancer Tyrosine Kinase Inhibitors Clinical Pipeline by Company, Indication &
Phase

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• Global Cancer Tyrosine Kinase Inhibitors Clinical Pipeline: 411 Drugs
• Majority of Cancer Tyrosine Kinase Inhibitors in Preclinical Phase: 164 Drugs
• Marketed Cancer Tyrosine Kinase Inhibitors: 32 Drugs
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Table of Contents
1. The Journey: Genesis to Present of Tyrosine Kinase Inhibitors
2. Tyrosine Kinase: An Overview
3. Tyrosine Kinases Inhibitors: Promising Tools for Targeted Cancer Therapies
4. Types of Tyrosine Kinase Receptors
4.1 Epidermal Growth Factor Receptor
4.1.1 Types of Epidermal Growth Factor Receptor
4.1.2 Epidermal Growth Factor Receptor & Ligands
4.1.3 Epidermal Growth Factor Receptor & Cancers
4.2 Platelet-Derived Growth Factor Receptor (PDGFR)
4.2.1 Types of Platelet-Derived Growth Factor Receptor
4.2.2 Platelet-Derived Growth Factor Receptor & Ligands
4.2.3 Platelet-Derived Growth Factor Receptor & Cancer
4.3 Insulin-Like Growth Factor 1 Receptor (IGF-1R)
4.3.1 Insulin-Like Growth Factor 1 Receptor & its Ligands
4.3.2 Insulin-Like Growth Factor 1 Receptor & its role in Cancer

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5. Signaling Pathway of Receptor Tyrosine Kinase
5.1 PI3K/Akt Pathway
5.2 Ras/Raf/ERK1/2 Pathway
5.3 The JAK/STAT Pathway
6. Advantage of Tyrosine Kinase Inhibitors for Treatment of Cancer
7. BCR-ABL Tyrosine Kinase Inhibitors
7.1 Imatinib
7.2 Nilotinib
7.3 Dasatinib
7.4 Ponatinib
7.5 Bosutinib
8. Epidermal Growth Factor Receptor Kinase Inhibitors Tyrosine
8.1 Gefitinib
8.2 Erlotinib
8. 3 Lapatinib
8.4 Icotinib
8.5 Canertinib
8.6 Afatinib
8.7 Neratinib
8.8 Poziotinib
9. Vascular Endothelial Growth Factor Tyrosine Kinase Inhibitors
9.1 Sunitinib
9.2 Sorafenib

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9.3 Vandetanib
9.4 Pazopanib
9.5 Axitinib
9.6 Cediranib
10. Applications of Tyrosine Kinase Inhibitor in Cancer Therapy
10.1 Role of Tyrosine Kinase Inhibitors in the First-Line Treatment of Advanced Non-Small
Cell Lung Cancer
10.2 Mitigation of Chronic Myeloid Leukaemia
10.3 Role of tyrosine Kinase Inhibitors in Combating Colorectal Cancer
10.4 Gastrointestinal Cancer & Tyrosine Kinase Inhibitor
10.5 Tyrosine Kinase Inhibitor in Breast Cancer
11. Global Tyrosine Kinase Inhibitors Market Overview
11.1 Current Market Scenario
11.2 Cancer Tyrosine Kinase Inhibitors Pipeline Overview
12. Global Tyrosine Kinase Inhibitor Market Dynamics
12.1 Favorable Driving Factors
12.1.1 Research & Development
12.1.2 Strong Clinical Pipeline
12.1.3 Increasing Disease Incidences
12.1.4 Unmet Requirement of Completely Curative Agents
12.1.5 Advancement in Manufacturing Capabilities of the Biopharmaceutical Companies
12.2 Challenges Countered by Tyrosine Kinase Inhibitor Market
12.2.1 Strict Regulatory Guidelines for Approval of Prospective Drug
12.2.2 Long Phase of Research & Development
12.2.3 Funding of Clinical Trials

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12.2.4 Highly Competitive Market
13. Global Tyrosine Kinase Inhibitor Market Future Prospects
14. Global Cancer Tyrosine Kinase Inhibitors Clinical Pipeline by Company, Indication &
Phase
14.1 Unknown
14.2 Research
14.3 Preclinical
14.4 Clinical
14.5 Phase-I
14.6 Phase-I/II
14.7 Phase-II
14.8 Phase-II/III
14.9 Phase-III
14.10 Preregistration
14.11 Registered
15. Marketed Cancer Tyrosine Kinase Inhibitors Clinical Insight by Brand Name,
Company & Indication
15.1 Blood Cancer
15.1.1 Ibrutinib (Imbruvica)
15.1.2 Ponatinib (Iclusig)
15.1.3 Dasatinib (Tasigna)
15.1.4 Nilotinib (Tasigna)
15.1.5 Bosutinib (Bosulif)
15.1.6 Radotinib (Supect)
15.2 Breast Cancer

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15.2.1 Trastuzumab Subcutaneous (Herceptin SC)
15.2.2 Pertuzumab (Omnitarg & Perjeta)
15.2.3 Lapatinib (Tykerb & Tyverb)
15.2.4 Trastuzumab Biosimilar (CANMAb & Hertraz)
15.2.5 Trastuzumab Biosimilar (Vivitra)
15.3 Gastric Cancer
15.3.1 Apatinib
15.4 Non-small cell lung cancer
15.4.1 Afatinib (Gilotrif, Giotrif & Tomtovok)
15.4.2 Nintedanib (Ofev & Vargatef)
15.4.3 Ceritinib (Zykadia)
15.4.4 Crizotinib (Xalkori)
15.4.5 Icotinib (Conmana)
15.4.6 Gefitinib (Iressa)
15.4.7 Alectinib (Alecensa)
15.5 Renal Cancer
15.5.1 Axitinib (Inlyta)
15.6 Thyroid Cancer
15.6.1 Vandetanib (Caprelsa, Zactima & Zictifa)
15.7 Multiple
15.7.1 Sunitinib (Sutent)
15.7.2 Lenvatinib (Lenvima)
15.7.3 Regorafenib (Stivarga)
15.7.4 Imatinib (Gleevec, Glivec & Ruvise)

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15.7.5 Trastuzumab (Herceptin)
15.7.6 Erlotinib (Tarceva)
15.7.7 Ramucirumab (Cyramza)
15.7.8 Cabozantinib (COMETRIQ, Cabometyx & Cometriq)
15.7.9 Nimotuzumab (BIOMAb EGFR, CIMAher, Cimaher, Taixinsheng, TheraCIM,
Theraloc & VECTHIX)
15.7.10 Sorafenib (Nexavar)
15.7.11 Imatinib (Imatib)
16. Discontinued & Suspended Cancer Tyrosine Kinase Inhibitors Clinical Pipeline by
Company & Phase
16.1 No Development Reported
16.2 Discontinued
16.3 Suspended
17. Competitive Landscape
17.1 AB Science
17.2 Advenchen Laboratories
17.3 Array BioPharma
17.4 ARIAD Pharmaceuticals
17.5 Astellas Pharma (OSI Pharmaceuticals)
17.6 AstraZeneca
17.7 Bayer HealthCare
17.8 Biocad
17.9 Biocon
17.10 Boehringer Ingelheim
17.11 Bristol-Myers Squibb

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17.12 Celera Genomics Group
17.13 Celgene Corporation (Avila Therapeutics)
17.14 Celltrion
17.15 Chugai Pharmaceutical
17.16 Cytopia Research
17.17 Daiichi Sankyo (Ambit Biosciences Corporation)
17.18 Dyax
17.19 Eisai Co Ltd
17.20 Exelixis
17.21 GlaxoSmithKline
17.22 Hanmi Pharmaceutical
17.23 Novartis
17.24 Onyx Pharmaceuticals
17.25 Pfizer
17.26 Plexxikon
17.27 Reliance Life Sciences
17.28 Roche
17.29 Shire
17.30 Synthon
17.31 Wyeth
17.32 Xcovery
17.33 Zydus Cadila

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List of Figures
Figure 3-1: Pictorial View of Signaling Pathways Involved on Activation of Tyrosine Kinase
Receptor
Figure 4-1: Different Types of Tyrosine Kinase Receptors
Figure 5-1: Various Possible Signaling Pathways Taken by Receptor Tyrosine Kinase
Figure 5-2: Steps Involved in PI3K/Akt Pathway
Figure 5-3: Signaling Pathway Followed by Ras/Raf/ERK1/2 Pathway
Figure 5-4: Signaling Pathway of JAK STAT Tyrosine Kinase Receptors
Figure 10-1: Applications of Tyrosine Kinase Inhibitors in Cancer Therapy
Figure 11-1: Global Cancer Kinase Inhibitors Market Opportunity (US$ Billion), 2015-2020
Figure 11-2: Global Cancer Tyrosine Kinase Inhibitors Clinical Pipeline by Phase (%), 2016
Figure 11-3: Global Cancer Tyrosine Kinase Inhibitors Clinical Pipeline by Phase (Numbers),
2016
Figure 11-4: Global Cancer Tyrosine Kinase Inhibitors Clinical Pipeline by Phase (%), 2016
Figure 11-5: Global Cancer Tyrosine Kinase Inhibitors Clinical Pipeline by Phase (Numbers),
2016
Figure 12-1: Various Driving Factors Involved in Establishment of Tyrosine Kinase Inhibitor
Market
Figure 12-2: List of the Drugs In Different Phases of Clinical Trials
Figure 12-3: List of Main Challenges Which Hamper Development of Tyrosine Kinase Inhibitors
Figure 17-1: AB Scicence - Clinical Pipeline
Figure 17-2: Advenchen Laboratories - Clinical Pipeline
Figure 17-3: ARIAD - Clinical Pipeline
Figure 17-4: Biocon - linical Pipeline

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Figure 17-5: Celgene Corporation - Clinical Pipeline
Figure 17-6: Daiichi Sankyo - Clinical Pipeline
Figure 17-7: Novartis - Clinical Pipeline
Figure 17-8: Plexxikon - Clinical Pipeline
Figure 17-9: Roche - Clinical Pipeline
Figure 17-10: Zydus Cadila - Clinical Pipeline
Table 3-1: Recently Approved Tyrosine Kinase Inhibitors
Table 4-1: ErbB Family Members & Their Ligands
Table 4-2: Platelet-Derived Growth Factor Receptor & Ligands
Table 4-3: Receptor Platelet Derived Tyrosine Kinase & the Cancers Associated
Table 4-4: Insulin Receptor Family Members & Its Ligands
Table 7-1: List of Tyrosine Kinase Inhibitors Developed against BCR-ABL Receptors
Table 8-1: List of the Drugs Targeting EFGR Receptor
Table 9-1: Different Drugs associated with The Treatment of Angiogenesis Related Cancers
Table 10-1: Tyrosine Kinase Inhibitors Targeting Lung Cancer
Table 10-2: Drugs being Developed to Treat Hematological Malignancies
Table 10-3: Drugs Used to Manage Breast Cancer
Table 10-4: Some of the Tyrosine Kinase Inhibitors Developed to Treat Metastatic Melanoma
Table 11-1: Drugs to Enter the Market in Near Future
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